首页|Enhanced oral bioavailability and intestinal lymphatic transport of a hydrophilic drug using liposomes.

Enhanced oral bioavailability and intestinal lymphatic transport of a hydrophilic drug using liposomes.

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A liposome system was evaluated for oral delivery of a poorly bioavailable hydrophilic drug。 The system was prepared from proliposome, which consisted of negatively charged phosphatidylcholine, whereas cefotaxime was chosen as the model drug。 An in vivo study was carried out on nine rats according to a three-way crossover design to compare the oral bioavailability of cefotaxime from the liposomal formulation with that of an aqueous drug solution and a physical mixture of cefotaxime with blank liposomes。 The results indicated that the extent of bioavailability of cefotaxime was increased approximately 2。7 and 2。3 times compared with that of the aqueous solution and the physical mixture, respectively。 In a separate study, simultaneous determination of cefotaxime in intestinal lymph (collected from the mesenteric lymph duct) and in plasma (collected from the tail vein) revealed that its concentration was consistently higher in the lymph than in the plasma when administered via the liposomal formulation, whereas the reverse was observed with the aqueous solution。 Thus, the results indicated that the liposomes system has the potential of increasing the oral bioavailability of poorly bioavailable hydrophilic drugs and also promote their lymphatic transport in the intestinal lymph。

OralLiposomesCefotaximeBiological AvailabilityLymph脂质体头孢噻肟生物利用度淋巴

Ling SS、Magosso E、Khan NA、Yuen KH、Barker SA

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School of Pharmaceutical Sciences, University of Science, Malaysia, Penang, Malaysia.

2006

Drug development and industrial pharmacy

Drug development and industrial pharmacy

SCI
ISSN:0363-9045
年,卷(期):2006.32(3)